Category: 620-20-2

Birgul, Kaan published the artcileSynthesis and molecular modeling of MetAP2 of thiosemicarbazides, 1,2,4-triazoles, thioethers derived from (S)-Naproxen as possible breast cancer agents, Recommanded Product: 3-Chlorobenzylchloride, the publication is Journal of Molecular Structure (2022), 132739, database is CAplus.

New thiosemicarbazides, 1,2,4-triazoles and thioethers I (R¹ = Ph, 4-FC₆H₄, Bn, etc.; R² = Bn, 3-FC₆H₄CH₂, 4-MeOC₆H₄CH₂, etc.) from derived (S)-Naproxen were synthesized in this study. The mol. binding of the compounds on MetAP-2 was performed. Anticancer effects of the synthesized compounds were studied by using MTT assay method on MCF-7 (includes estrogen and progesterone receptors) and MDA-MB-231 (lacks estrogen and progesterone receptors) adenocarcinoma cell lines at 0, 10, 25, 50, 75 and 100μM concentrations for 24 h. The IC₅₀ values of novel (S)-Naproxen derivatives were determined between from 5 to 100μM on MCF-7 breast cancer cell line and MDA-MB-231 cell lines. The apoptotic activity of selected compounds I (R¹ = 4-ClC₆H₄; R² = 3-FC₆H₄CH₂) and I (R¹ = Ph; R² = 4-MeC₆H₄CH₂) were first analyzed by Annexin V staining using Tali Image-Based Cytometer. Mitochondrial membrane potential changes determined in fluorescence plate reader following JC-1 stain for compounds I (R¹ = 4-ClC₆H₄; R² = 3-FC₆H₄CH₂) and I (R¹ = Ph; R² = 4-MeC₆H₄CH₂) in MCF-7 and MDA-MB-231 cells. The effect of these compounds on the cell viability 4T1 mouse mammary tumor cell line was tested at 1 to 5 times of calculated IC₅₀ value (IC₅₀x1, IC₅₀x2, IC₅₀x3, IC₅₀x4, and IC₅₀x5). Next in order to determine the toxicity of the combination of compound I (R¹ = Bn; R² = 3-FC₆H₄CH₂) and Docetaxel, WST-1 cell viability and proliferation assay was performed with 4T1.

Journal of Molecular Structure published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C7H6Cl2, Recommanded Product: 3-Chlorobenzylchloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Aghcheli, Ayoub published the artcileDesign, synthesis, and biological evaluation of 1-(5-(benzylthio)-1,3,4-thiadiazol-2-yl)-3-phenylurea derivatives as anticancer agents, Recommanded Product: 3-Chlorobenzylchloride, the publication is Medicinal Chemistry Research, database is CAplus.

Abstract: A novel series of 1-(5-(benzylthio)-1,3,4-thiadiazol-2-yl)-3-phenylurea derivatives (5a-l) were designed and synthesized as sorafenib analogs. The in vitro cytotoxicity effects of synthesized compounds were evaluated against four different human cancer cells including MCF-7, HepG2, A549, and HeLa cell lines. The biol. results showed that most of the compounds significantly prevented the proliferation of tested cancer cells. In particular, 2-F, 4-Cl, and 2,6-diF substituted derivatives (5d, 5g, and 5k) showed promising activities, especially against Hela cancer cells (IC₅₀ = 0.37, 0.73 and 0.95 μM, resp.) which were significantly more potent than sorafenib as the reference drug (IC₅₀ = 7.91 μM). Flow cytometry anal. revealed that the prototype compounds (5d, 5g, and 5k) significantly induced apoptotic cell death in HeLa cancer cells and blocked the cell cycle at the sub-G1 phase. Moreover, in silico docking study confirmed the binding of the prototype compound to the active site of VEGFR-2.

Medicinal Chemistry Research published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C7H6Cl2, Recommanded Product: 3-Chlorobenzylchloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kim, Minsoo published the artcileStructure activity relationship exploration of 5-hydroxy-2-(3-phenylpropyl)chromones as a unique 5-HT_2B receptor antagonist scaffold, Computed Properties of 620-20-2, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(21), 127511, database is CAplus and MEDLINE.

Antagonists for the serotonin receptor 2B (5-HT_2B) have clin. applications towards migraine, anxiety, irritable bowl syndrome, and MDMA abuse; however, few selective 5-HT_2B antagonists have been identified. Previous studies from these labs identified a natural product, 5-hydroxy-2-(2-phenylethyl)chromone (5-HPEC, 2) as the first non-nitrogenous ligand for the 5-HT_2B receptor. Studies on 5-HPEC optimization led to the identification of 5-hydroxy-2-(3-phenylpropyl)chromone (5-HPPC, 3), which showed a tenfold improvement in binding affinity over 2 at 5-HT_2B. This study aimed to further improve receptor pharmacol. of this unique scaffold. Guided by mol. modeling studies modifications at the C-3′ and C-4′ positions of 3 were made to probe their effects on ligand binding affinity and efficacy. Among the derivatives synthesized 5-hydroxy-2-(3-(3-cyanophenyl)propyl)chromone (5-HCPC, 3d) showed the most promise with a multifold improvement in binding affinity (pK_i = 7.1 ± 0.07) over 3 with retained antagonism.

Bioorganic & Medicinal Chemistry Letters published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C7H6Cl2, Computed Properties of 620-20-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Bhattacherjee, Debojit published the artcileTrisulfides over disulfides: highly selective synthetic strategies, anti-proliferative activities and sustained H₂S release profiles, Product Details of C7H6Cl2, the publication is Chemical Communications (Cambridge, United Kingdom) (2019), 55(90), 13534-13537, database is CAplus and MEDLINE.

Temperature- and solvent-induced selective synthesis of trisulfides and disulfides is demonstrated. A remarkable selectivity was achieved using Na₂S as a sulfur-transfer agent under mild, greener, catalyst-free and additive-free conditions. This study reveals trisulfides as a better model than disulfides in general for a sustained release of H₂S and potent anti-cancer activities.

Chemical Communications (Cambridge, United Kingdom) published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C7H6Cl2, Product Details of C7H6Cl2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Liu, Hongyan published the artcileSynthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents, Formula: C7H6Cl2, the publication is European Journal of Medicinal Chemistry (2019), 163-173, database is CAplus and MEDLINE.

Several series of novel tryptophan-derived rhodanine derivatives were synthesized and identified as potential competitive PTP1B inhibitors and antibacterial agents. Among the compounds studied, I [R = 4-Br] was found to have the best in vitro inhibition activity against PTP1B (IC₅₀ = 0.36 ± 0.02 μM). In addition, the compounds also showed potent inhibition against other PTPs, especially CDC25B. Mol. docking anal. demonstrated that compounds II and I [R = 4-Br] could occupy both the catalytic site and the adjacent pTyr binding site simultaneously. The compounds also showed higher levels of activity against gram-pos. strains, the gram-neg. strain Escherichia coli 1924, and multidrug-resistant gram-pos. bacterial strains. Compounds II, III, IV and I [R = 4-Me, 4-F] had comparable or more potent antibacterial activity than the pos. controls.

European Journal of Medicinal Chemistry published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C7H6Cl2, Formula: C7H6Cl2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Yang, Xi published the artcileDihydropyrimidinone imidazoles as unique structural antibacterial agents for drug-resistant gram-negative pathogens, Recommanded Product: 3-Chlorobenzylchloride, the publication is European Journal of Medicinal Chemistry (2022), 114188, database is CAplus and MEDLINE.

The health crisis caused by severe multidrug resistance increasingly compels the exploitation of new alternative antibacterial drugs. A library of structurally unique dihydropyrimidinone imidazoles as novel potential antibacterial agents was developed with the aim to confront drug resistance. Some target compounds exhibited strong antibacterial activities, especially, sulfamethoxazole hybridized dihydropyrimidinone imidazole 8b was found to be extremely active against multidrug-resistant K. pneumonia and A. baumanii at a low concentration of 0.5 μg/mL, which outperformed norfloxacin even clinafloxacin. This active compound not only exhibited low cytotoxicity to mammalian cells (human red blood cells, HepG2 and ECs), but also possessed rapid bactericidal property, good biofilm inhibition ability, and a low propensity to induce K. pneumonia and A. baumanii resistance. Further studies revealed that the inhibitory effect of the active compound 8b might be achieved by disrupting membrane integrity, increasing ROS generation, reducing GSH activity and interacting with DNA. These findings provided a bright hope for developing dihydropyrimidinone imidazoles to combat emergent drug resistance.

European Journal of Medicinal Chemistry published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C17H14F3N3O2S, Recommanded Product: 3-Chlorobenzylchloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Li, Shaochen published the artcileNon-food bioactive products: Semisynthesis, biological activities, and mechanisms of action of oximinoether derivatives of matrine from Sophora flavescens, Application In Synthesis of 620-20-2, the publication is Industrial Crops and Products (2019), 134-141, database is CAplus.

Matrine, a quinolizidine alkaloid isolated from the roots of Sophora flavescens, is a naturally non-food bioactive product. To discover new non-food bioactive product-based pesticides, a series of 15-chloro-18-oximinoether derivatives of matrine were prepared by structural modifications of matrine. Compounds 7 m, 7o, 7q, 7 s, and 7 t display potent insecticidal activity against Mythimna separata Walker. Compounds 7b (R² = n-butyl) and 7 l (R² = p-methylbenzyl) exhibit greater than 6 folds more pronounced acaricidal activity than matrine against Tetranychus cinnabarinus Boisduval. Through reverse transcription polymerase chain reaction (RT-PCR) and quant. real-time polymerase chain reaction (qRT-PCR) anal., it is found that introduction of the chlorine atom and the oximinoether moiety at the C-15 and C-18 positions of matrine is important for acting with nAChR α1, α2 and α4 subunits in T. cinnabarinus; α1, α2, α4 and β3 subunits may be the target of action of compound 7b against T. cinnabarinus; structural modification on the lactam ring of compound 1 can lead to the change of mode of action on VGSC in T. cinnabarinus.

Industrial Crops and Products published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C7H6Cl2, Application In Synthesis of 620-20-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Tang, Xu published the artcileSynthesis and bioactivity evaluation of penta-1,4-diene-3-one oxime ether derivatives, Application of 3-Chlorobenzylchloride, the publication is Journal of Pesticide Science (Tokyo, Japan) (2019), 44(4), 242-248, database is CAplus and MEDLINE.

A series of penta-1,4-diene-3-one oxime ether derivatives I (R = 2,4-Cl₂C₆H₃, 4-MeOC₆H₄, 6-Cl-3-pyridyl, etc.; X = 4-OBn, 2-OBn) were synthesized, and their antiviral and antifungal activities were evaluated. Bioactivity evaluations showed that most target compounds had significant antiviral activity against tobacco mosaic virus (TMV). The synthesized compounds also showed certain inhibitory effects on three plant-pathogenic fungi, but all of them are lower than that of the control drug epoxiconazole. Among them, I (R = 3-FC₆H₄; X = 4-OBn) was found to have good curative activity against TMV, with an inhibition rate of 64.6%, which was better than that of ribavirin (45.2%). Compound I (R = 6-Cl-3-pyridyl; X = 4-OBn) had a remarkable protective effect against TMV, with an inhibitory rate of 66.9%, which was better than that of ribavirin (61.8%). The inhibitory rate of compound I (R = 4-ClC₆H₄; X = 2-OBn) in inactivation activity against TMV was 87.0%, which was better than that of ribavirin (77.9%). Further mol. docking studies indicated that compound I (R = 4-ClC₆H₄; X = 2-OBn) showed strong binding affinities toward the coat protein of tobacco mosaic virus. This result indicates that penta-1,4-diene-3-one oxime ether derivatives can play a significant role in discovering new antiviral agents.

Journal of Pesticide Science (Tokyo, Japan) published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C10H11NO4, Application of 3-Chlorobenzylchloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Fu, Dong-Jun published the artcileDiscovery of novel tertiary amide derivatives as NEDDylation pathway activators to inhibit the tumor progression in vitro and in vivo, SDS of cas: 620-20-2, the publication is European Journal of Medicinal Chemistry (2020), 112153, database is CAplus and MEDLINE.

NEDDylation pathway regulates multiple physiol. process, unlike inhibitors, NEDDylation activators are rarely studied. Novel amide derivatives were synthesized and evaluated for antiproliferative activity against MGC803, MCF-7 and PC-3 cells. Among them, VII-31 displayed the most potent activity with an IC₅₀ value of 94 nmol/L against MGC803 cells. Cellular mechanisms elucidated that VII-31 inhibited the cell viability, arrested cell cycle at G2/M phase and induced apoptosis via intrinsic and extrinsic pathways against MGC803 cells. In addition, VII-31 activated NAE1-Ubc12-Cullin1 NEDDylation via interacting with NAE1 directly. Furthermore, the activation of NEDDylation resulted in the degradation of inhibitor of apoptosis proteins (IAPs). Importantly, VII-31 inhibited tumor growth in xenograft models in vivo without the apparent toxicity. In summary, it is the first time to reveal that VII-31 deserves consideration for cancer therapy as a NEDDylation activator.

European Journal of Medicinal Chemistry published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C7H6Cl2, SDS of cas: 620-20-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Du, Haitang published the artcileSynthesis and fungicidal activity of 3-[5-(substituted thio)-4H-1,2,4-triazol-3-yl]-benzopyran-2-ones, Category: chlorides-buliding-blocks, the publication is Huaxue Tongbao (2019), 82(9), 831-836, 854, database is CAplus.

In order to find triazole lead compounds with fungicidal activity, a series of new triazole derivatives containing coumarin ring and thioether structure were synthesized by the introduction of coumarin ring and thioether structural unit into mols. of triazoles. They were structurally confirmed by ¹H NMR, ¹³C NMR, IR, MS and elemental anal. The preliminary bioactivity test showed that some of the target compounds have certain fungicidal activity at the test concentration

Huaxue Tongbao published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C7H6Cl2, Category: chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics